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71. 发明授权

US4328135A Octapeptides lowering growth hormone 失效
标题翻译：八肽降低生长激素
公开(公告)号：US4328135A
公开(公告)日：1982-05-04
申请号：US233813
申请日：1981-02-12
申请人： Dimitrios Sarantakis
发明人： Dimitrios Sarantakis
IPC分类号： A61K38/00 , C07K14/655 , C08L37/00
CPC分类号： C07K14/6555 , A61K38/00 , Y10S930/12
摘要： Polypeptides of the formula: ##STR1## in which X.sub.1 is Phe, D-Phe or C.sub.6 H.sub.5 CH.sub.2 CH.sub.2 CO--;X.sub.2 is Phe, Tyr, Trp, Met or Leu;X.sub.3 is Trp or D-Trp;X.sub.4 is Thr, Val, .alpha.-Abu or Phe;andX.sub.5 is Phe, D-Phe or --NHCH.sub.2 CH.sub.2 C.sub.6 H.sub.3 ;the linear precursor intermediates thereof and pharmaceutically acceptable salts and amides thereof are selective inhibitors of growth hormone release without materially altering blood serum levels of glucagon or insulin. In addition, the above-described compounds are active growth hormone suppressants for periods as long as two hours.
摘要翻译：其中X1是Phe，D-Phe或C6H5CH2CH2CO-的下式的多肽：; X2是Phe，Tyr，Trp，Met或Leu; X3是Trp或D-Trp; X4是Thr，Val，α-Abu或Phe; X5为Phe，D-Phe或-NHCH2CH2C6H3; 其线性前体中间体和其药学上可接受的盐和酰胺是生长激素释放的选择性抑制剂，而不会显着改变胰高血糖素或胰岛素的血清水平。此外，上述化合物是活性生长激素抑制剂长达两个小时。

72. 发明授权

US4320118A Deca-, undeca-, dodeca- and tridecapeptides with thymic activity 失效
标题翻译：十二烷基，十一碳环十二烷和十三肽具有胸腺活性
公开(公告)号：US4320118A
公开(公告)日：1982-03-16
申请号：US218886
申请日：1980-12-22
申请人： Abraham White, deceased , John J. Nestor , Gordon H. Jones , Pamela M. Burton
发明人： Abraham White, deceased , John J. Nestor , Gordon H. Jones , Pamela M. Burton
IPC分类号： C07K7/08 , A61K38/00 , C07K7/06 , C07K14/655 , A61K37/00 , C07C103/52
CPC分类号： C07K14/6555 , A61K38/00 , Y10S930/18
摘要： Novel peptides of the formula: ##STR1## wherein: A, A' and A" are each independently Gly, D-Ala, D-Leu, or D-Trp, wherein A may optionally be N-alkylated or N-acylated;B is Pro, .DELTA..sup.3 -Pro, Thz, or diMeThz;C and C' are each independently Thr, Ser, Val, or alloThr;D is Glu, Gln, Asp, or Asn;R is hydrogen, or is lower alkyl or lower acyl, substituted for one of the hydrogens on the .epsilon.-amino group of the lysyl residue;X is Cys, Ala, ABU, or Cys(Me); andY is selected from the group consisting of hydroxy, Pro, Pro-Leu, and Pro-Leu-Met, -NH.sub.2, ProNH.sub.2, Pro-LeuNH.sub.2 and Pro-leu-MetNH.sub.2 ;and the pharmaceutically acceptable salts thereof, are useful for increasing immunologic competence. Methods for preparation of the peptides are also described.
摘要翻译：下式的新型肽：其中：A，A'和A“各自独立地为Gly，D-Ala，D-Leu或D-Trp，其中A可以任选地被N-烷基化或N-酰化; B是Pro，DELTA 3-Pro，Thz或diMeThz; C和C'各自独立地为Thr，Ser，Val或AlloThr; D是Glu，Gln，Asp或Asn; R是氢，或者是低级烷基或低级酰基，取代赖氨酰残基的ε-氨基上的氢之一; X是Cys，Ala，ABU或Cys（Me）; 并且Y选自羟基，Pro，Pro-Leu和Pro-Leu-Met，-NH 2，ProNH 2，Pro-LeuNH 2和Pro-leu-MetNH 2; 及其药学上可接受的盐可用于增加免疫能力。还描述了肽的制备方法。

73. 发明授权

US4310518A Cyclic hexapeptide somatostatin analogs 失效
公开(公告)号：US4310518A
公开(公告)日：1982-01-12
申请号：US192776
申请日：1980-10-01
申请人： Roger M. Freidinger , Daniel F. Veber
发明人： Roger M. Freidinger , Daniel F. Veber
IPC分类号： A61K38/00 , C07K14/655 , A61K37/00 , C07C103/52
CPC分类号： C07K14/6555 , A61K38/00 , Y10S514/806 , Y10S930/16
摘要： Somatostatin analogs are prepared wherein a cyclic hexapeptide contains a secondary amino acid which replaces seven of the ring amino acids of somatostatin. The cyclic hexapeptides are easier to synthesize, have a longer duration of activity, and many have a greater level of activity than somatostatin. The compounds have the properties of inhibiting the release of glucagon, growth hormone and insulin. Certain of the compounds also are capable of inhibiting the release of gastric acid secretions. The compounds are particularly useful in the treatment of acromegaly, diabetes, diabetic retinopathy and peptic ulcers. These cyclic hexapeptides are prepared by the solid phase method.

74. 发明授权

US4291022A Organic compounds 失效
标题翻译：有机化合物
公开(公告)号：US4291022A
公开(公告)日：1981-09-22
申请号：US152706
申请日：1980-05-23
申请人： Edmond Sandrin , Wilfried Bauer
发明人： Edmond Sandrin , Wilfried Bauer
IPC分类号： A61K38/00 , C07K5/083 , C07K5/103 , C07K14/655 , A61K37/00 , C07C103/52
CPC分类号： C07K14/6555 , C07K5/0808 , C07K5/1005 , A61K38/00 , Y10S514/806 , Y10S930/16 , Y10S930/26
摘要： This invention provides new compounds of formula I, ##STR1## wherein R.sub.1, X, Y and Z are amino acid residues andeach B is hyrogen or together are a bond,useful as growth hormone secretion inhibitors.
摘要翻译：本发明提供了新的式I化合物，其中R1，X，Y和Z是氨基酸残基，每个B是氢或一起是可用作生长激素分泌抑制剂的键。

75. 发明授权

US4259234A Analgesic compounds 失效
标题翻译：止痛化合物
公开(公告)号：US4259234A
公开(公告)日：1981-03-31
申请号：US807849
申请日：1977-06-20
申请人： Edward L. Smithwick, Jr. , Robert C. A. Frederickson , Robert T. Shuman
发明人： Edward L. Smithwick, Jr. , Robert C. A. Frederickson , Robert T. Shuman
IPC分类号： A61K38/00 , A61K38/08 , A61P25/04 , C07K1/107 , C07K7/06 , C07K14/575 , C07K14/655 , C07K14/70 , C07C103/52
CPC分类号： C07K14/702 , A61K38/00 , Y10S514/809
摘要： Compounds of the formula ##STR1## and pharmaceutically acceptable non-toxic acid addition salts thereof, in which L and D, when applicable, define the chirality;R.sub.1 is hydrogen, C.sub.1 -C.sub.3 primary alkyl, or allyl;R.sub.2 is hydrogen or C.sub.1 -C.sub.3 primary alkyl, subject to the limitation that when R.sub.1 is allyl, R.sub.2 is hydrogen;R.sub.3 is hydrogen or C.sub.1 -C.sub.3 primary alkyl;R.sub.4 is C.sub.1 -C.sub.4 primary or secondary alkyl;R.sub.5 is hydrogen or C.sub.1 -C.sub.4 primary or secondary alkyl;R.sub.6 is hydrogen or C.sub.1 -C.sub.3 primary alkyl;R.sub.7 is hydrogen or C.sub.1 -C.sub.3 primary alkyl;Y is hydrogen or acetyl;Z is hydrogen of ##STR2## in which R.sub.8 is C.sub.1 -C.sub.3 alkyl or hydrogen; and W is isopropyl, --VR.sub.9, or --CH.sub.2 --X--CH.sub.3, in which V is O or S, R.sub.9 is C.sub.1 -C.sub.4 alkyl or aralkyl, and X is O, S, or --CH.sub.2 --, subject to the limitation that, when W is isopropyl, R.sub.7 is C.sub.1 -C.sub.3 primary alkyl; are useful analgesic agents.
摘要翻译：其中L和D在适用时限定手性;式 R1是氢，C1-C3伯烷基或烯丙基; R 2为氢或C 1 -C 3伯烷基，但受限于当R 1为烯丙基时，R 2为氢; R3是氢或C1-C3伯烷基; R4是C1-C4伯或仲烷基; R5是氢或C1-C4伯或仲烷基; R6是氢或C1-C3伯烷基; R 7是氢或C 1 -C 3伯烷基; Y是氢或乙酰基; Z是的氢，其中R8是C1-C3烷基或氢; 并且W是异丙基，-VR 9或-CH 2 -X-CH 3，其中V是O或S，R 9是C 1 -C 4烷基或芳烷基，X是O，S或-CH 2 - ，其受限于当W是异丙基时，R 7是C 1 -C 3伯烷基; 是有用的止痛剂。

76. 发明授权

US4256736A Psychopharmacological peptides 失效
标题翻译：精神药理学肽
公开(公告)号：US4256736A
公开(公告)日：1981-03-17
申请号：US14081
申请日：1979-02-22
申请人： David de Wied , Hendrik M. Greven
发明人： David de Wied , Hendrik M. Greven
IPC分类号： C07K14/655 , A61K38/00 , A61P25/00 , A61P25/20 , C07K1/113 , C07K14/575 , C07K14/67 , C07K14/675 , A61K37/00 , C07C103/52
CPC分类号： C07K14/672 , C07K14/6755 , A61K38/00
摘要： Novel and biologically useful peptides of the formula: A.sub.1 -A.sub.2 -L-Phe-X-L-Thr-L-Ser-R.sub.1 -Y-L-Ser-R.sub.2 -L-Thr-L-Pro-L-Leu-L-Val-L-Thr-B are disclosed (together with pharmaceutical compositions comprising a pharmaceutically effective amount of same) wherein:(a) A.sub.1 and A.sub.2 each represent an aminoacid residue of the formula H.sub.2 N-ALK-CO-, where ALK is an alkylidene group with 1 to 6 carbon atoms inclusively;(b) X is an amino-acid residue selected from the group consisting of L-Met, L-Met(O), L-Met(O.sub.2) and L-Leu;(c) R.sub.1 and R.sub.2 each represent one of the amino-acid residues selected from the group consisting of L-Glu and L-Gln;(d) Y represents an amino acid residue selected from the group consisting of L-Lys and D-Lys; and(e) B represents one of the amino-acid or peptide moieties selected from L-Leu-OH, D-Leu-OH, L-Leu-L-Phe-OH, L-Leu-L-Phe-L-Lys-OH, L-Leu-L-Phe-D-Lys-OH, L-leucinol and L-MeLeu-OHor a functional derivative thereof; these peptides have psychopharmacological properties capable of accelerating the inhibition of the conditioned flight response, so that they are eminently suitable for the treatment of certain mental disorders in which reduction of the brain function is desired; more particularly the peptides have neuroleptic activity. Peptides of formula (I) wherein one of R.sub.1 and R.sub.2 is L-Glu and the other L-Gln are preferred, and compositions containing compositions of formula (I) wherein R.sub.1 is L-Glu and R.sub.2 is L-Gln are especially suitable.
摘要翻译：具有下式的新颖和生物有用的肽：A1-A2-L-Phe-XL-Thr-L-Ser-R1-YL-Ser-R2-L-Thr-L-Pro-L-Leu-L-Val-L 公开了-Thr-B（与包含药学上有效量的药物组合物），其中：（a）A1和A2各自表示式H2N-ALK-CO-的氨基酸残基，其中ALK是具有1个亚烷基的氨基酸残基至6个碳原子; （b）X是选自L-Met，L-Met（O），L-Met（O 2）和L-Leu的氨基酸残基; （c）R1和R2各自表示选自L-Glu和L-Gln的氨基酸残基之一; （d）Y表示选自L-Lys和D-Lys的氨基酸残基; 和（e）B代表选自L-Leu-OH，D-Leu-OH，L-Leu-L-Phe-OH，L-Leu-L-Phe-L-Lys的氨基酸或肽部分之一 -OH，L-Leu-L-Phe-D-Lys-OH，L-亮氨醇和L-MeLeu-OH或其功能衍生物; 这些肽具有能够加速对条件飞行反应的抑制的精神药理学特性，使得它们非常适合于治疗某些需要降低脑功能的精神障碍; 更具体地，肽具有精神抑制活性。其中R1和R2中的一个是L-Glu，另一个L-Gln是优选的式（I）的肽，并且含有其中R 1是L-Glu和R 2是L-Gln的式（I）的组合物的组合物是特别合适的。

77. 发明授权

US4235886A Cyclic hexapeptide somatostatin analogs 失效
标题翻译：循环六肽生长抑素类似物
公开(公告)号：US4235886A
公开(公告)日：1980-11-25
申请号：US89827
申请日：1979-10-31
申请人： Roger M. Freidinger , Daniel F. Veber
发明人： Roger M. Freidinger , Daniel F. Veber
IPC分类号： C07K7/64 , A61K38/00 , A61K38/04 , A61P1/04 , A61P3/08 , A61P3/10 , A61P5/02 , A61P27/02 , A61P43/00 , C07K1/06 , C07K1/113 , C07K14/575 , C07K14/655 , A61K37/00 , C07C103/52
CPC分类号： C07K14/6555 , A61K38/00 , Y10S514/806 , Y10S930/16
摘要： Somatostatin analogs are prepared wherein a cyclic hexapeptide contains a secondary amino acid which replaces seven of the ring amino acids of somatostatin. The cyclic hexapeptides are easier to synethesize, have a longer duration of activity, and many have a greater level of activity than somatostatin. The compounds have the properties of inhibiting the release of glucagon, growth hormone and insulin. Certain of the compounds also are capable of inhibiting the release of gastric acid secretions. The compounds are particularly useful in the treatment of acromegaly, diabetes, diabetic retinopathy and peptic ulcers. These cyclic hexapeptides are prepared by the solid phase method.
摘要翻译：制备生长抑素类似物，其中环状六肽含有替代生长抑素的七个环氨基酸的仲氨基酸。环状六肽更易于整合，具有更长的活性持续时间，并且许多具有比生长抑素更高的活性水平。该化合物具有抑制胰高血糖素，生长激素和胰岛素释放的性质。某些化合物还能够抑制胃酸分泌物的释放。该化合物特别可用于治疗肢端肥大症，糖尿病，糖尿病性视网膜病变和消化性溃疡。这些环状六肽通过固相法制备。

78. 发明授权

US4231923A Assay method and compounds 失效
标题翻译：测定方法和化合物
公开(公告)号：US4231923A
公开(公告)日：1980-11-04
申请号：US841678
申请日：1977-10-13
申请人： Richard J. Miller , Kwen-Jen Chang , Pedro Cuatrecasas
发明人： Richard J. Miller , Kwen-Jen Chang , Pedro Cuatrecasas
IPC分类号： C07K14/655 , A61K51/00 , A61K51/08 , C07B31/00 , C07B59/00 , C07C67/00 , C07K1/113 , C07K14/575 , C07K14/67 , C07K14/70 , C07C103/52 , A61K43/00
CPC分类号： C07K14/702 , A61K51/08 , C07K14/672 , A61K2123/00 , Y10S436/804 , Y10S436/808 , Y10S514/809
摘要： The present invention provides an assay method for opioid activity comprising the steps of:(a) incubating together an opiate receptor material, a radio-iodinated structural analogue of leucine-enkephalin or methionine-enkephalin, and a liquid sample;(b) measuring the percentage inhibition of the binding of the radio-iodinated compound to the opiate receptor material; and(c) determining the opioid activity of the liquid sample using the percentage inhibition measurement.Also provided are a test kit of value in the performance of such assays, and novel compounds of use in such assays together with methods for their preparation.
摘要翻译：本发明提供了一种阿片类活性测定方法，包括以下步骤：（a）将阿片剂受体材料，亮氨酸 - 脑啡肽或甲硫氨酸 - 脑啡肽的放射碘化结构类似物和液体样品一起孵育; （b）测量放射碘化化合物与阿片剂受体材料结合的抑制百分比; 和（c）使用抑制百分比测量来确定液体样品的阿片样物质活性。还提供了在这种测定的性能中有价值的测试试剂盒，以及在这些测定中使用的新型化合物及其制备方法。

79. 发明授权

US4215039A Somatostatin analogues 失效
标题翻译：生长抑素类似物
公开(公告)号：US4215039A
公开(公告)日：1980-07-29
申请号：US12430
申请日：1979-02-15
申请人： Dimitrios Sarantakis
发明人： Dimitrios Sarantakis
IPC分类号： A61K38/00 , C07K14/655 , C07C103/52 , C07G7/00
CPC分类号： C07K14/6555 , A61K38/00 , Y10S514/806 , Y10S930/16
摘要： X.sub.4 is Arg, His or Lys;X.sub.5 is His, Tyr or Glu;X.sub.8 is Trp or D-Trp;X.sub.10 is Val, .alpha.-Abu, Leu, Phe or Tyr; andX.sub.14 is Cys, D-Cys or --NH(CH.sub.2).sub.2 --S--,inhibit the release of growth hormone and glucagon without substantial decrease in insulin and are useful in the treatment of acromegaly and diabetes.
摘要翻译：其中X 2是H，NH 2，Ala-Gly-，Ala-D-Ala-，Gly-Gly-Gly-，低级烷酰基或苯甲酰基; X4是Arg，His或Lys; X5是His，Tyr或Glu; X8是Trp或D-Trp; X10是Val，α-Abu，Leu，Phe或Tyr; X14是Cys，D-Cys或-NH（CH2）2-S-，抑制生长激素和胰高血糖素的释放，而胰岛素没有显着降低，可用于治疗肢端肥大症和糖尿病。

80. 发明授权

US4204990A Somatostatin analogues 失效
标题翻译：生长抑素类似物
公开(公告)号：US4204990A
公开(公告)日：1980-05-27
申请号：US895577
申请日：1978-04-12
申请人： Dimitrios Sarantakis
发明人： Dimitrios Sarantakis
IPC分类号： A61K38/00 , C07K14/655 , C07C103/52 , A61K37/00
CPC分类号： C07K14/6555 , A61K38/00 , Y10S514/806 , Y10S930/16
摘要： Polypeptides of the formula: ##STR1## the linear precursors and non-toxic acid addition salts thereof, wherein: R is hydrogen, lower alkanoyl, benzoyl, Ala-Gly-, Gly-Gly-Gly-, Ala-D-Ala- or p-Glu;X.sub.4 is Arg or Lys;X.sub.5 is a D-.alpha.-amino acid;X.sub.8 is L-Trp or D-Trp; andX.sub.14 is Cys or D-Cysare described. These somatostatin analogues are useful as inhibitors of growth hormone and insulin secretion, selectively inhibiting growth hormone, insulin and glucagon and they demonstrate prolonged growth hormone inhibition for periods exceeding two hours. The compounds of this invention are useful in the treatment of diabetes, acromegaly and other dysfunctions characterized by excessive secretion of growth hormone and/or insulin.
摘要翻译：下式的多肽：其中：R是氢，低级烷酰基，苯甲酰基，Ala-Gly-，Gly-Gly-Gly-，Ala- D-Ala-或p-Glu; X4是Arg或Lys; X5是D-α-氨基酸; X8是L-Trp或D-Trp; X14是Cys或D-Cys。这些生长抑素类似物可用作生长激素和胰岛素分泌的抑制剂，选择性抑制生长激素，胰岛素和胰高血糖素，并且它们在超过两小时的时间内表现出延长的生长激素抑制。本发明的化合物可用于治疗以生长激素和/或胰岛素过度分泌为特征的糖尿病，肢端肥大症和其他功能障碍。

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